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Epirubicin HCl.

Epirubicin hydrochloride 是阿霉素的半合成的 L-阿拉伯糖衍生物，能够抑制 Topoisomerase，起到抗肿瘤的作用。

目录号: PC10263 纯度: ≥98%

CAS No. :56390-09-1

商品编号	规格	价格	会员价
PC10263-5mg	5mg	¥441.00	请登录
PC10263-25mg	25mg	¥1764.00	请登录
PC10263-100mg	100mg	¥3528.00	请登录
PC10263-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥627.20	请登录

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中文名称	Epirubicin HCl.
中文别名	盐酸表阿霉素;盐酸表柔比星;4'-表阿霉素盐酸盐;表柔比星杂质;表柔霉素;外延盐酸多柔比星;盐酸阿霉素;盐酸表阿霉素标准品;盐酸表柔比星； Epirubicin HCl;盐酸表柔比星 EP标准品;盐酸表柔比星；盐酸表阿霉素;盐酸表柔比星(比星类);盐酸表柔比星；盐酸表阿霉素;(8S,10S)-10-[(3'-氨基-2',3',6'-三脱氧-alpha-L-阿拉伯吡喃糖基)-O-]-6,8,11-三羟基-8-羟乙酰基-1-甲氧基-7,8,9,10-四氢并四苯-5,12-二酮盐酸盐
英文名称	Epirubicin HCl
英文别名	Epirubicin HCl;epirubicin hydrochloride;l-erythro-dihydrosphingosine;4'-Epidoxorubicin hydrochloride;5,12-Naphthacenedione, 10-[(3-amino-2,3,6-trideoxy-.α.-L-arabino-hexopyranosyl)oxy]-7,8,9,10-tetrahydro-6,8,11-trihydroxy-8-(hydroxyacetyl)-1-methoxy-, hydrochloride;Epirubicin (hydrochloride);Epirubicin, Hydrochloride Salt (4'-Epidoxorubicin,Pharmorubicin®, Ellence®, Epirubicin Ebewe®, Pharmorubicin,Ridorubicin);(8S-cis)-10-[(3-Amino-2,3,6-trideoxy-alpha-L-arabino-hexopyranosyl)oxy]-7,8,9,10-tetrahydro-6,8,11-trihydroxy-8-(hydroxyacetyl)-1-methoxynaphthacene-5,12-dione hydrochloride;(7S,9S)-7-[(2R,4R,5R)-4-Amino-5-hydroxy-6-methyloxan-2-yl]oxy-6,9,11-trihydroxy-9-(2-hydroxyacetyl)-
Cas No.	56390-09-1
分子式	C₂₇H₃₀ClNO₁₁
分子量	579.98
包装储存	4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

生物活性

Epirubicin hydrochloride (4-Epidoxorubicin hydrochloride), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin hydrochloride inhibits DNA and RNA synthesis. Epirubicin hydrochloride is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.

性状

Solid

IC50 & Target[1][2]

Topoisomerase

体外研究(In Vitro)

Epirubicin hydrochloride (4-Epidoxorubicin hydrochloride), like doxorubicin, exerts its antitumor effects by complex with DNA, resulting in damage to DNA and interference with the synthesis of DNA, RNA, and proteins. Epirubicin hydrochloride may also affect the integrity and activity of cellular membranes. Maximal cell kill caused by Epirubicin hydrochloride occurs during the S phase of the cell cycle. With higher concentrations effects are also seen in early G2 as well as G1 and M phases.
Epirubicin hydrochloride display antineoplastic activity against most cancer cells. Epirubicin hydrochloride is cytotoxic to Hepatoma G2 cells with IC₅₀ of 1.6 μg/mL at 24 hr. 1.6 μg/mL Epirubicin hydrochloride induces apoptosis of Hep G2 cells, and higher activity of catalase by 50%, Se-dependent glutathione peroxidase by 110%, Cu, Zn-superoxide dismutase by 172% and Mn-superoxide dismutase by 135%. Epirubicin hydrochloride increases the cellular expression of NADPH-CYP 450 reductase, and reduces GST-π expression.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Epirubicin hydrochloride (4-Epidoxorubicin hydrochloride) are clinically active against a broad range of tumor types, including breast cancer, malignant lymphomas, soft tissue sarcomas, lung cancer, pleural mesothelioma, gastrointestinal cancer, head and neck cancer, ovarian cancer, prostatic carcinoma, transitional bladder carcinoma and so on.
Epirubicin hydrochloride at a dose of 3.5 mg/kg suppresses tumor mass of human breast tumor xenograft R-27 by 74.4 %.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

ClinicalTrial

参考文献

[1]. Cersosimo RJ, et al. Epirubicin: a review of the pharmacology, clinical activity, and adverse effects of an adriamycin analogue. J Clin Oncol. 1986 Mar;4(3):425-39. [Information]

[2]. Kashima H, et al. Epirubicin, Identified Using a Novel Luciferase Reporter Assay for Foxp3 Inhibitors, Inhibits Regulatory T Cell Activity. PLoS One. 2016 Jun 10;11(6):e0156643. [Information]

[3]. Ozkan, A., et al. Epirubicin HCl toxicity in human-liver derived hepatoma G2 cells. Pol J Pharmacol, 2004. 56(4): p. 435-44. [Information]

[4]. Bonadonna, G., et al. Drugs ten years later: epirubicin. Ann Oncol, 1993. 4(5): p. 359-69. [Information]

[5]. Asanuma, F., et al. Antitumor activity of paclitaxel and epirubicin in human breast carcinoma, R-27. Folia Microbiol (Praha), 1998. 43(5): p. 473-4. [Information]

溶解度数据

体外研究:

H₂O : 50 mg/mL (86.21 mM; Need ultrasonic)

DMSO : 25 mg/mL (43.10 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7242 mL	8.6210 mL	17.2420 mL
5 mM	0.3448 mL	1.7242 mL	3.4484 mL
10 mM	0.1724 mL	0.8621 mL	1.7242 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 2.5 mg/mL (4.31 mM); Clear solution
2.

建议依照次序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.31 mM); Clear solution
3.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (3.59 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.59 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
4.

建议依照次序添加每种溶剂： PBS
Solubility: 1.1 mg/mL (1.90 mM); Clear solution; Need ultrasonic
5.

建议依照次序添加每种溶剂： 1% DMSO 99% saline
Solubility: ≥ 0.5 mg/mL (0.86 mM); Clear solution

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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